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Synthesis and biological evaluation of 5-arylamino-6-chloro-1H-indazole-4,7-diones as inhibitors of protein kinase B/Akt

DOI: 10.1016/j.bmcl.2006.08.120
Title: Synthesis and biological evaluation of 5-arylamino-6-chloro-1H-indazole-4,7-diones as inhibitors of protein kinase B/Akt
Journal Title: Bioorganic & Medicinal Chemistry Letters
Volume: 16
Issue: 23
Publication Date: 1 December 2006
Start Page: 6001
End Page: 6005
Published online: online 20 September 2006
ISSN: 0960-894X
Affiliations:

  • a College of Pharmacy, Ewha Womans University, Seodaemun-ku, Seoul 120-750, Republic of Korea

  • b ILDONG Research Laboratories, ILDONG Pharmaceutical Co. Ltd., 260-5, Eonnam-Dong, Kuseong-Gu, Yongin, Kyongki-Do 449-910, Republic of Korea
  • Abstract: of 5-arylamino-6-chloro-1H-indazole-4,7-diones were synthesized and evaluated for their inhibitory activity on protein kinase B/Akt. The compounds exhibited a potent Akt1 inhibitory activity. Further mechanistic study revealed that they might have dual inhibitory effects on both activity and phosphorylation of Akt1 in PC-3 tumor cell line.
    Accepted: 30 August 2006
    Received: 7 July 2006
    Revised: 14 August 2006
    Keywords: Akt; Inhibitor; 1H-indazole-4,7-dione; Antitumor
    Corresponding information:
    Tel: +82 2 3277 3027
    Fax: +82 2 3277 3051
    Email: ckryu@ewha.ac.kr

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